Non-steroidal anti-inflammatory drugs (NSAIDs) are considered to be the first-line drugs in the symptomatic treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac is one of the emerging NSAID molecules for arthritis treatment. It is a newer derivative of diclofenac and has less gastrointestinal complications.
Primary mechanism responsible for its anti-inflammatory, antipyretic, and analgesic action is inhibition of prostaglandin synthesis by inhibition of cyclooxygenase (COX). Inhibition of COX also decreases prostaglandins in the epithelium of the stomach, making it more sensitive to corrosion by gastric acid. This is also the main side-effect of diclofenac. Diclofenac has a low to moderate preference to block the COX2-isoenzyme (approximately 10-fold) and is said to have, therefore, a somewhat lower incidence of gastrointestinal complaints than noted with indomethacin and aspirin. Aceclofenac has higher anti-inflammatory action than conventional NSAIDs and this is a cytokine inhibitor. Aceclofenac works by blocking the action of a substance in the body called cyclo-oxygenase. Aceclofenac is essentially a phenyl acetic acid derivative and inhibits interleukin1b-induced prostaglandin E2 production but has poor COX-I inhibitor effect in oral form. Cyclo-oxygenase is involved in the production of various chemicals in the body, some of which are known as prostaglandins. Prostaglandins are produced in response to injury or certain diseases and would otherwise go on to cause pain, swelling and inflammation. In this respect, Arthritic conditions are one such example.
As long-term use of diclofenac and similar NSAIDs predisposes for peptic ulcer, many patients are at risk for this complication.
Presently, both Aceclofenac and Diclofenac are available commercially in the form of immediate release or sustained release tablets, capsules, gels, but injection formulations are available as only as immediate release as described by the Inventor's Indian Patent No. 236996.
Sustained release formulations of Aceclofenac and Diclofenac are commercially available in the form of film coated tablets, Capsules and gel.
Moreover, even though use of different means such as polymer, solvent or matrix has been proposed in the past for enhancing effectiveness of NSAIDs, there still remain challenges in terms of optimum drug loading in to solvent system, optimization size and stabilization drugs loaded system and to control and release of NSAIDS at a predefined and reproducible rate for prolonged period.